KU-55933

Cas No.:	587871-26-9
Chemical Name:	2-Morpholino-6-(thianthren-1-yl)-4H-pyran-4-one
Synonyms:	2-Morpholin-4-yl-6-thianthren-1-ylpyran-4-one;KU-55933 (ATM Kinase Inhibitor);2-Morpholino-6-(thianthren-1-yl)-4H-pyran-4-one;KU 55933;Ku-55933;KU-55933 (KU 55933, KU55933);Name: KU-55933;2-Morpholin-4-yl-6-thianthren-1-yl-pyran-4-one;2-Thianthren-1-yl-6-morpholin-4-yl-pyran-4-one;ATM Kinase Inhibitor;2-(4-Morpholinyl)-6-(1-thianthrenyl)-4H-Pyran-4-one;2-(Morpholin-4-yl)-6-(thianthren-1-yl)-4H-pyran-4-one;KU55933;O549494L5D;2-morpholino-6-thianthren-1-yl-pyran-4-one;4H-Pyran-4-one, 2-(4-morpholinyl)-6-(1-thianthrenyl)-;PubChem22474;GTPL5928;2-Thian
SMILES:	S1C2=C([H])C([H])=C([H])C([H])=C2SC2=C([H])C([H])=C([H])C(=C12)C1=C([H])C(C([H])=C(N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])O1)=O
Formula:	C21H17NO3S2
M.Wt:	395.4946
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

In Vitro:

KU-55933 (10 μM) blocks the ionizing radiation-induced p53 serine 15 phosphorylation. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with an estimated IC50 of 300 nM. KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 specifically inhibits ATM but not the other DNA damage-activated PIKKs, ATR, and DNA-PK[1]. KU-55933 induces pATM, p53, E2F1 and pATR, noticeably upregulates the nuclear fraction of E2F1 at the 0.5 h time point[2]. Metformin increases ATM and AMPK phosphorylation, as well as SHP protein level in primary hepatocytes, and this stimulatory effect of metformin is repressed by a specific ATM kinase inhibitor KU-55933[3].